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[Absorption of recombinant hirudin in rats GI tract]
Xue-ying Yan1, Xue-nong Zhang, Qiang Zhang
1Department of Pharmaceutics, School of Pharmaceutical Science, Peking University, Beijing 100083, China.
Aim:
To investigate the absorption and distribution of recombinant hirudin-2 (rHV2) in the GI tract in rats after oral administration.
Methods:
Using HPLC, fluorescence spectrophotometry and confocal laser scanning microscopy to measure the amount of intact rHV2 absorbed into gastrointestinal mucosa and blood.
Results:
HPLC spectrum showed that there were intact rHV2 molecules in plasma after 1 h of oral administration. After oral administration for 3 h, 1.2%-26.8% of fluorescence was found in the GI tract in rats. Chromatographic analysis showed that 2.27%-38.75% of fluorescence recovered from the GI tract luminal contents and mucosa was eluted at the void volume of a Sephadex G-25 column. Microscopic examination showed that FITC-rHV2 was taken up throughout the whole small intestine but the ileum appeared to be a preferred site for FITC-rHV2 transport in rats.
Conclusion:
rHV2 may partially survive in the GI lumen and subsequently absorbed in active form by gastrointestinal tract.
